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Assay Detail

CHEMBL750800

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Binding potency for Norepinephrine transporter using [3H]NE
11
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Norepinephrine transporter (CHEMBL304)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

3 alpha-(4'-substituted phenyl)tropane-2 beta-carboxylic acid methyl esters: novel ligands with high affinity and selectivity at the dopamine transporter.
Holmquist CR, Keverline-Frantz KI, Abraham P, Boja JW, Kuhar MJ, Carroll FI.
J Med Chem (1996) 39 : 4139 -4141
PubMed 8863789 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.58 7.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL14391 2 7.44
CHEMBL306208 2 7.43
CHEMBL82027 2 7.22
CHEMBL2079586 2 6.08
CHEMBL1790051 2 6.04
CHEMBL370805 COCAINE 4.0 1 5.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL14391 IC50 = 36.0 nM 7.44
CHEMBL306208 IC50 = 37.0 nM 7.43
CHEMBL14391 IC50 = 52.4 nM 7.28
CHEMBL306208 IC50 = 60.1 nM 7.22
CHEMBL82027 IC50 = 60.0 nM 7.22
CHEMBL82027 IC50 = 275.0 nM 6.56
CHEMBL2079586 IC50 = 835.0 nM 6.08
CHEMBL1790051 IC50 = 920.0 nM 6.04
CHEMBL2079586 IC50 = 1230.0 nM 5.91
CHEMBL1790051 IC50 = 2080.0 nM 5.68
CHEMBL370805 COCAINE IC50 = 3298.0 nM 5.48